• Bulletin of the Korean Chemical Society
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• 제32권4호
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• pp.1249-1252
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• 2011

Inhibition of BACE 1 activity is considered as a promising therapeutic target for Alzheimer's Disease (AD). Synthesis and inhibitory activities of (4-arylpiperazinyl)piperidines by bioisosteric replacement of a biaryl group with an arylpiperazine as BACE 1 inhibitors are described. The resulting (4-arylpiperazinyl)piperidines represent novel nonpeptide BACE 1 inhibitors with improved in vitro potency.

• Toxicological Research
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• 제17권
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• pp.89-96
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• 2001

Recently, considerable attention has been focused on the role of cyclooxygenase-2 (COX-2) in the carcinogenesis as well as in inflammation. Improperly overexpressed COX-2 has been observed in many types of human cancers and transformed cells in culture. Thus, it is conceivable that targeted inhibition of abnormally or improperly up-regulated COX-2 provides one of the most effective and promising strategies for cancer prevention. A ubiquitous eukaryotic transcription factor, NF-kB is considered to be involved in regulation of COX-2 expression. Furthermore, extracellular-regulated protein kinase and p38 mitogen-activated protein (MAP) kinase appear to be key elements of the intracellular signaling cascades involved in NF-kB activation in response to a wide array of external stimuli. Certain chemopreventive phytochemicals suppress activation of NF-kB by blocking one or more of the MAP kinases, which may contribute to their inhibitory effects on COX-2 induction. One of the plausible mechanisms by which chemopreventive phytochemicals inhibit NF-kB activation involves suppression of degradation of the inhibitory unit I kB, which hampers subsequent translocation of p65, the functionally active subunit of NF-kB.

• 한국가시화정보학회지
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• 제14권1호
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• pp.27-32
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• 2016

The reduction of $CO_2$ emissions has been a key target in the Marine Industry since the IMO's Marine Environment Protection Committee published its findings in 2009. The representative emission index is termed as the EEDI (Energy Efficiency Design Index) for the new ships. Among various flow control techniques ever proposed, the air lubrication method is the one of most promising one in terms of practical applicability. The present study examines the basic characteristics of the flat plate test with intention of applying the air lubrication technology to the reduction of the resistance of a ship. Image analysis technique is proposed as a tool to quantify the effectiveness of the air lubrication method.

• 한국미생물·생명공학회지
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• 제32권1호
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• pp.1-10
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• 2004

Many bacteria monitor their population density and control the expression of specialized gene sets in response to bacterial cell density based on a mechanism referred to as quorum sensing. In all cases, quorum sensing involves the production and detection of extracellular signaling molecules, auto inducers, as which Gram-negative and Gram-positive bacteria use most prevalently acylated homoserine lactones and processed oligo-peptides, respectively. Through quorum-sensing communication circuits, bacteria regulate a diverse array of physiological functions, including virulence, symbiosis, competence, conjugation, antibiotic production, motility, sporulation, and biofilm formation. Many pathogens have evolved quorum-sensing mechanisms to mount population-density-dependent attacks to over-whelm the defense responses of plants, animals, and humans. Since these AHL-mediated signaling mechanisms are widespread and highly conserved in many pathogenic bacteria, the disruption of quorum-sensing system might be an attractive target for novel anti-infective therapy. To control AHL-mediated pathogenicity, several promising strategies to disrupt bacterial quorum sensing have been reported, and several chemicals and enzymes have been also investigated for years. These studies indicate that anti-quorum sensing strategies could be developed as possible alternatives of antibiotics.

• 통합자연과학논문집
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• 제4권3호
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• pp.216-221
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• 2011

c-Jun N-terminal kinase-3 (JNK-3) has been shown to mediate neuronal apoptosis and make the promising therapeutic target for neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and other CNS disorders. In order to better understand the structural and chemical features of JNK-3, comparative molecular field analysis (CoMFA) was performed on a series of 3,5-disubstituted quinolines derivatives. The best predictions were obtained CoMFA model ($q^2$=0.707, $r^2$=0.972) and the statistical parameters from the generated 3D-QSAR models were indicated that the data are well fitted and have high predictive ability. The resulting contour map from 3D-QSAR models might be helpful to design novel and more potent JNK3 derivatives.

• 대한전자공학회:학술대회논문집
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• 대한전자공학회 2003년도 신호처리소사이어티 추계학술대회 논문집
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• pp.557-560
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• 2003

Voice is one of the promising biometrics because it is one of the most convenient ways human would distinguish someone from others. The target of speaker verification is to divide the client from imposters. Support Vector Machine(SVM) is in the limelight as a binary classifier, so it can work well in speaker verification. In this paper, we combined SVM with genetic algorithm(GA) to reduce the dimensionality of input feature. Experiments were conducted with Korean connected digit database using different feature dimensions. The verification accuracy of SVM with GA is slightly lower than that of SVM, but the proposed algorithm has greater strength in the memory limited systems.

• 한국환경보건학회지
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• 제29권3호
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• pp.1-8
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• 2003

The development of environmentally nontoxic or non-polluting antifouling additives that can be formulated in practical coating requires assay involving target organisms. Described here are the simple laboratory assays that have been developed using the barnacle, Balanus amphitrite, a common fouling organism found throughout temperate and tropical seas. One of the assays depends on synchronous year-round mass culture, the procedure for which is described, of nauplii larvae and cyprids larvae. The laboratory assays provided quantitative estimates of toxicity and settlement inhibition of the test compounds. Laurinterol (1), isolaurinterol (2), alpysinal (3), and aplysin (4) have been isolated from the Korean red alga Laurencia okamurae. Their structures were identified by spectral data in comparison with the literature data. Compounds 1-4 inhibited larval settlement of the barnacle B. amphitrite with EC$_{50}$ values of 0.18- 36 $\mu\textrm{g}$/ml. Com-pounds 2-4 showed larval toxicity against nauplii of the barnacle B. amphitrite with 5-10 $\mu\textrm{g}$/ml, while laurinterol (1) exhibited no toxicity at even 100 $\mu\textrm{g}$/ml. Therefore, laurinterol was expected as a promising natural antifoulant.t.

• Molecules and Cells
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• 제41권1호
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• pp.65-72
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• 2018

Autophagy is an evolutionally conserved cytoplasmic degradation system in which varieties of materials are sequestered by a double membrane structure, autophagosome, and delivered to the lysosomes for the degradation. Due to the wide varieties of targets, autophagic activity is essential for cellular homeostasis. Recent genetic evidence indicates that autophagy has a crucial role in the regulation of animal lifespan. Basal level of autophagic activity is elevated in many longevity paradigms and the activity is required for lifespan extension. In most cases, genes involved in autophagy and lysosomal function are induced by several transcription factors including HLH-30/TFEB, PHA-4/FOXA and MML-1/Mondo in long-lived animals. Pharmacological treatments have been shown to extend lifespan through activation of autophagy, indicating autophagy could be a potential and promising target to modulate animal lifespan. Here we summarize recent progress regarding the role of autophagy in lifespan regulation.

• Biomolecules & Therapeutics
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• 제24권5호
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• pp.453-468
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• 2016

There is a conserved ATPase domain in topoisomerase II (topo II) and heat shock protein 90 (Hsp90) which belong to the GHKL (gyrase, Hsp90, histidine kinase, and MutL) family. The inhibitors that target each of topo II and Hsp90 are intensively studied as anti-cancer drugs since they play very important roles in cell proliferation and survival. Therefore the development of dual targeting anti-cancer drugs for topo II and Hsp90 is suggested to be a promising area. The topo II and Hsp90 inhibitors, known to bind to their ATP binding site, were searched. All the inhibitors investigated were docked to both topo II and Hsp90. Four candidate compounds as possible dual inhibitors were selected by analyzing the molecular docking study. The pharmacophore model of dual inhibitors for topo II and Hsp90 were generated and the design of novel dual inhibitor was proposed.

• 대한핵의학회지
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• 제38권2호
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• pp.205-208
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• 2004

The two major classes of magnetic resonance (MR) contrast agents are paramagnetic contrast agents, usually based on chelates of gadolinium generating T1 positive signal enhancement, and super-paramagnetic contrast agents that use mono- or polycrystalline iron oxide to generate strong T2 negative contrast in MR images. These paramagnetic or super-paramagnetic complexes are used to develop new contrast agents that can target the specific molecular marker of the cells or tan be activated to report on the physiological status or metabolic activity of biological systems. In molecular imaging science, MR imaging has emerged as a leading technique because it provides high-resolution three-dimension maps of the living subject. The future of molecular MR imaging is promising as advancements in hardware, contrast agents, and image acquisition methods coalesce to bring high resolution in vivo imaging to the biochemical sciences and to patient care.